Solubility and dissolution enhancement of eplerenone by using nanoprecipitation technique

The present study aimed to increase the Solubility and Dissolution rate of Eplerenone by formulation of Eplerenone nanosuspension by using nanoprecipitation technique. Poor solubility and slow dissolution rate are major issues for the majority of upcoming drugs and existing biologically active compounds. Eplerenone is highly selective aldosterone blocker. It is used for treatment of hypertension and heart failure, but problem associated with its poor solubility in biological fluids. Eplerenone is BCS Class-II having low solubility and high permeability. All the Eplerenone nanosuspension formulations (F1 to F12) were characterization for its Particle size and its distribution, Zeta potential analysis, Scanning Electron Microscopy, Drug excipients interactions investigated by using FT-IR examinations, Entrapment Efficiency (EE) and in vitro release kinetics. The optimized formulation (F12) showed an average particle size and zeta potential is 179.05 nm and -55 mV respectively. The dissolution rate for the optimized nanosuspension was enhanced (97.05 % in 45 min) relative to pure Eplerenone (30 % in 60 min), mainly due to the formulation of nanosized particles. Stability study revealed that nanosuspension was more stable at room and refrigerator condition with no significant change in particle size distribution. These results indicate that the Eplerenone loaded Nanosuspension significantly improved in-vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect.